HRP20210655T1 - 3-methyl-pyrrolidine-2,5-dione derivatives useful as cgrp receptor antagonists - Google Patents

3-methyl-pyrrolidine-2,5-dione derivatives useful as cgrp receptor antagonists Download PDF

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Publication number
HRP20210655T1
HRP20210655T1 HRP20210655TT HRP20210655T HRP20210655T1 HR P20210655 T1 HRP20210655 T1 HR P20210655T1 HR P20210655T T HRP20210655T T HR P20210655TT HR P20210655 T HRP20210655 T HR P20210655T HR P20210655 T1 HRP20210655 T1 HR P20210655T1
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Croatia
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compound
hydrate
salt
methyl
compound according
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HRP20210655TT
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Croatian (hr)
Inventor
Jennifer Anne Mcmahon
Miles Goodman Siegel
Russell Dean Stucky
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Eli Lilly And Company
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Publication of HRP20210655T1 publication Critical patent/HRP20210655T1/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Claims (17)

1. Spoj, naznačen time što ima formulu: [image] , ili farmaceutski prihvatljiva sol, ili njegov hidrat.1. Compound, characterized by having the formula: [image] , or a pharmaceutically acceptable salt, or a hydrate thereof. 2. Spoj ili sol u skladu s patentnim zahtjevom 1, naznačen time što ima formulu: [image] , ili njegov hidrat.2. A compound or salt according to claim 1, characterized in that it has the formula: [image] , or its hydrate. 3. Spoj ili sol u skladu s bilo patentnim zahtjevom 1 ili patentnim zahtjevom 2, naznačen time što ima formulu: [image] , ili njegov hidrat.3. A compound or salt according to either claim 1 or claim 2, characterized in that it has the formula: [image] , or its hydrate. 4. Spoj ili sol u skladu s patentnim zahtjevom 3, naznačen time što je: [image] .4. Compound or salt according to claim 3, characterized in that: [image] . 5. Spoj u skladu s patentnim zahtjevom 4, naznačen time što je: [image] .5. Compound according to patent claim 4, characterized in that: [image] . 6. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (3S)-3-[(1R)-1-[4-[(2-ciklopropil-6-metil-4-piridil)oksimetil]fenil]etil]-3-metilpirolidin-2,5-dion-hidroklorid, ili njegov hidrat.6. A compound according to claim 1, characterized in that (3S)-3-[(1R)-1-[4-[(2-cyclopropyl-6-methyl-4-pyridyl)oxymethyl]phenyl]ethyl] -3-methylpyrrolidine-2,5-dione hydrochloride, or its hydrate. 7. Spoj u skladu s patentnim zahtjevom 6, naznačen time što je (3S)-3-[(1R)-1-[4-[(2-ciklopropil-6-metil-4-piridil)oksimetil]fenil]etil]-3-metilpirolidin-2,5-dion-hidroklorid monohidrat.7. A compound according to claim 6, characterized in that (3S)-3-[(1R)-1-[4-[(2-cyclopropyl-6-methyl-4-pyridyl)oxymethyl]phenyl]ethyl] -3-methylpyrrolidine-2,5-dione hydrochloride monohydrate. 8. Spoj u skladu s patentnim zahtjevom 7, naznačen time što je spoj kristalan.8. A compound according to claim 7, characterized in that the compound is crystalline. 9. Spoj u skladu s patentnim zahtjevom 8, naznačen time ima maksimum u spektru difrakcije rendgenskih zraka na prahu pod kutom difrakcije 2θ od 26,3° u kombinaciji s jednim ili više maksimuma koje se bira iz skupine koju čine 13,8°, 22,2°, 19,7°, 21,3°, 14,1°, te 25,4°, uz toleranciju za kutove difrakcije od 0,2 stupnjeva.9. The compound according to claim 8, characterized by having a maximum in the X-ray powder diffraction spectrum at a diffraction angle 2θ of 26.3° in combination with one or more maxima selected from the group consisting of 13.8°, 22 ,2°, 19.7°, 21.3°, 14.1°, and 25.4°, with a tolerance for diffraction angles of 0.2 degrees. 10. Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (3S)-3-[(1R)-1-[4-[(2-ciklopropil-6-metil-4-piridil)oksimetil]fenil]etil]-3-metilpirolidin-2,5-dion-hidrobromid, ili njegov hidrat.10. Compound according to claim 1, characterized in that (3S)-3-[(1R)-1-[4-[(2-cyclopropyl-6-methyl-4-pyridyl)oxymethyl]phenyl]ethyl] -3-methylpyrrolidine-2,5-dione hydrobromide, or its hydrate. 11. Spoj u skladu s patentnim zahtjevom 10, naznačen time što je (3S)-3-[(1R)-1-[4-[(2-ciklopropil-6-metil-4-piridil)oksimetil]fenil]etil]-3-metilpirolidin-2,5-dion-hidrobromid monohidrat.11. A compound according to claim 10, characterized in that (3S)-3-[(1R)-1-[4-[(2-cyclopropyl-6-methyl-4-pyridyl)oxymethyl]phenyl]ethyl] -3-methylpyrrolidine-2,5-dione-hydrobromide monohydrate. 12. Spoj u skladu s patentnim zahtjevom 11, naznačen time što je spoj kristalan.12. A compound according to claim 11, characterized in that the compound is crystalline. 13. Spoj u skladu s patentnim zahtjevom 12, naznačen time ima maksimum u spektru difrakcije rendgenskih zraka na prahu pod kutom difrakcije 2θ od 26,1° u kombinaciji s jednim ili više maksimuma koje se bira iz skupine koju čine 13,9°, 22,1°, 8,7°, 19,5°, 18,8°, uz toleranciju za kutove difrakcije od 0,2 stupnjeva.13. The compound according to claim 12, characterized by having a maximum in the powder X-ray diffraction spectrum at a diffraction angle 2θ of 26.1° in combination with one or more maxima selected from the group consisting of 13.9°, 22 ,1°, 8.7°, 19.5°, 18.8°, with a tolerance for diffraction angles of 0.2 degrees. 14. Spoj ili sol, ili njegov hidrat, u skladu s bilo kojim od patentnih zahtjeva 1-13, naznačen time što je namijenjen upotrebi u terapiji.14. A compound or salt, or its hydrate, in accordance with any of claims 1-13, characterized in that it is intended for use in therapy. 15. Spoj ili sol, ili njegov hidrat, u skladu s bilo kojim od patentnih zahtjeva 1-13, naznačen time što je namijenjen upotrebi u liječenju migrene.15. A compound or salt, or its hydrate, in accordance with any of claims 1-13, characterized in that it is intended for use in the treatment of migraine. 16. Farmaceutski pripravak, naznačen time što sadrži spoj ili sol, ili njegov hidrat, u skladu s bilo kojim od patentnih zahtjeva 1-13, uz jedan ili više farmaceutski prihvatljivih nosača, razrjeđivača ili pomoćnih sredstava.16. Pharmaceutical preparation, characterized in that it contains a compound or salt, or its hydrate, in accordance with any of the patent claims 1-13, with one or more pharmaceutically acceptable carriers, diluents or auxiliary agents. 17. Postupak priprave farmaceutskog pripravka, naznačen time što se sastoji u miješanju spoja ili soli, ili njegovog hidrata, u skladu s bilo kojim od patentnih zahtjeva 1-13, s jednim ili više farmaceutski prihvatljivih nosača, razrjeđivača ili pomoćnih sredstava.17. Process for the preparation of a pharmaceutical preparation, characterized in that it consists in mixing the compound or salt, or its hydrate, in accordance with any of the patent claims 1-13, with one or more pharmaceutically acceptable carriers, diluents or auxiliaries.
HRP20210655TT 2017-05-15 2021-04-26 3-methyl-pyrrolidine-2,5-dione derivatives useful as cgrp receptor antagonists HRP20210655T1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762506204P 2017-05-15 2017-05-15
PCT/US2018/031526 WO2018213059A1 (en) 2017-05-15 2018-05-08 3-methyl-pyrrolidine-2,5-dione derivatives useful as cgrp receptor antagonists
EP18727529.2A EP3625221B1 (en) 2017-05-15 2018-05-08 3-methyl-pyrrolidine-2,5-dione derivatives useful as cgrp receptor antagonists

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HRP20210655T1 true HRP20210655T1 (en) 2021-05-28

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US (1) US10336726B2 (en)
EP (1) EP3625221B1 (en)
JP (1) JP6794583B2 (en)
CN (1) CN110662741B (en)
AR (1) AR111665A1 (en)
CA (1) CA3061762C (en)
CY (1) CY1124032T1 (en)
DK (1) DK3625221T3 (en)
ES (1) ES2870325T3 (en)
HR (1) HRP20210655T1 (en)
HU (1) HUE054448T2 (en)
LT (1) LT3625221T (en)
PL (1) PL3625221T3 (en)
PT (1) PT3625221T (en)
RS (1) RS61657B1 (en)
SI (1) SI3625221T1 (en)
TW (1) TW201904955A (en)
WO (1) WO2018213059A1 (en)

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EP3625220B1 (en) 2017-05-15 2021-03-10 Eli Lilly and Company Cgrp receptor antagonists
US20230096051A1 (en) * 2019-12-12 2023-03-30 Eli Lilly And Company Cgrp antigonists useful as tracer compounds for positron emission tomography
CN115704811B (en) * 2022-12-26 2023-03-31 南京威凯尔生物医药科技有限公司 Method for detecting ubjzepam and enantiomer and diastereomer impurities thereof by high performance liquid chromatography

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US6680387B2 (en) 2000-04-24 2004-01-20 Aryx Therapeutics Materials and methods for the treatment of diabetes, hyperlipidemia, hypercholesterolemia, and atherosclerosis
US9227972B2 (en) 2012-05-09 2016-01-05 Merck Sharp & Dohme Corp. Aliphatic spirolactam CGRP receptor antagonists
TWI636041B (en) 2015-08-12 2018-09-21 美國禮來大藥廠 Cgrp receptor antagonists
TW201718574A (en) 2015-08-12 2017-06-01 美國禮來大藥廠 CGRP receptor antagonists

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US20180327384A1 (en) 2018-11-15
LT3625221T (en) 2021-04-26
PT3625221T (en) 2021-04-15
EP3625221A1 (en) 2020-03-25
DK3625221T3 (en) 2021-04-19
ES2870325T3 (en) 2021-10-26
CA3061762C (en) 2021-11-09
JP6794583B2 (en) 2020-12-02
EP3625221B1 (en) 2021-03-03
TW201904955A (en) 2019-02-01
CA3061762A1 (en) 2018-11-22
WO2018213059A1 (en) 2018-11-22
CY1124032T1 (en) 2022-05-27
RS61657B1 (en) 2021-04-29
CN110662741B (en) 2022-08-16
PL3625221T3 (en) 2021-08-23
SI3625221T1 (en) 2021-04-30
JP2020519686A (en) 2020-07-02
HUE054448T2 (en) 2021-09-28
AR111665A1 (en) 2019-08-07
CN110662741A (en) 2020-01-07
US10336726B2 (en) 2019-07-02

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